BDBM100954 US10189794, Compound I-241::US10618902, Compound I-241::US10774052, Compound I-241::US9695132, I-241

SMILES CN1c2c(cnc(n2)N[C@@H]3COC[C@@H]3NC(=O)C=C)C=C(C1=O)c4c(c(cc(c4Cl)OC)OC)Cl

InChI Key InChIKey=ZIJVLVUPDVUSMA-UHFFFAOYSA-N

Data  8 IC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 8 hits for monomerid = 100954   

TargetFibroblast growth factor receptor 4(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of recombinant human wild type N-His tagged FGFR4 (460-802) using Y10-Sox as substrate in presence of 250 uM ATP by Omnia kinase methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetFibroblast growth factor receptor 4(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 8.80nMAssay Description:Inhibition of FGFR4 (unknown origin) expressed in human Huh7 cells assessed as autophosphorylation after 1 hr incubation measured by Mesoscale discov...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetFibroblast growth factor receptor 4(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 100nMAssay Description:A 10× stock solution of FGFR4-WT (PR4380C), (from Invitrogen, Carlsbad, Calif.) corresponding to method a in Table 7, was prepared as described below...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/25/2019
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetFibroblast growth factor receptor 4(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 100nMpH: 7.5Assay Description:Omnia Assay Protocol for Potency Assessment Against FGFR 4 Enzyme. a) [FGFR4-WT]=10 nM, [ATP]=300 uM, [Y10-Sox]=10 uM (ATP KMapp 300 uM): A 10x stock...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/19/2018
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetFibroblast growth factor receptor 4(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 100nMAssay Description:For MDA-MB-453 cells signaling, cells were grown in 96-well poly-D-lysine plates (BD Bioscience, San Jose, Calif.) to 90% confluence, and were then i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/25/2021
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetFibroblast growth factor receptor 4(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 500nMAssay Description:A 10× stock solution of FGFR4-WT (PR4380C or P3054), (from Invitrogen, Carlsbad, Calif.) corresponding to method a in Table 10, was prepared as descr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2020
Entry Details
US Patent
PDB3D3D Structure (crystal)
TargetFibroblast growth factor receptor 2(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 505nMAssay Description:Inhibition of recombinant human tagged FGFR2 using Y10-Sox as substrate in presence of 250 uM ATP by Omnia kinase methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetFibroblast growth factor receptor 2(Human)
Bristol Myers Squibb

Curated by ChEMBL
LigandPNGBDBM100954(US9695132, I-241 | US10189794, Compound I-241 | US...)
Affinity DataIC50: 842nMAssay Description:Inhibition of FGFR2 (unknown origin) expressed in KATO -III cells assessed as autophosphorylation after 1 hr incubation measured by Mesoscale discove...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed